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Compounds Interfering with Embryonic Lethal Abnormal Vision (ELAV) Protein-RNA Complexes: An Avenue for Discovering New Drugs

Nasti, R., Rossi, D., Amadio, M., Pascale, A., Unver, M. Y., Hirsch, A. K. H. & Collina, S., 26-Oct-2017, In : Journal of Medicinal Chemistry. 60, 20, p. 8257-8267 11 p.

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  • Compounds Interfering with Embryonic Lethal Abnormal Vision (ELAV) Protein − RNA Complexes: An Avenue for Discovering New Drugs

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DOI

  • Rita Nasti
  • Daniela Rossi
  • Marialaura Amadio
  • Alessia Pascale
  • M. Yagiz Unver
  • Anna K. H. Hirsch
  • Simona Collina

RNA-binding proteins play a key role in post-transcriptional processes. Among these proteins, embryonic lethal abnormal vision (ELAV) proteins are among the best described. ELAV proteins predominantly act as positive regulators of gene expression, and their dysregulation is involved in several pathologies, such as cancer, inflammation, and neurodegenerative diseases. Only a few structurally unrelated compounds interfering with ELAV protein-mRNA complexes have been identified by applying high-throughput screening approaches. Considering the structural diversity of the compounds discovered so far and the different techniques employed for screening their ability to interfere with ELAV protein-mRNA complexes, drawing conclusions from structure-activity relationships remains a challenge. We performed docking studies to understand the interactions of compounds reported over the past decade to be inhibitors of ELAV proteins and to evaluate the potential of computer-aided drug design to target this family of proteins for further drug discovery.

Original languageEnglish
Pages (from-to)8257-8267
Number of pages11
JournalJournal of Medicinal Chemistry
Volume60
Issue number20
Publication statusPublished - 26-Oct-2017

    Keywords

  • AU-RICH ELEMENT, MESSENGER-RNA, BINDING PROTEINS, ALZHEIMERS-DISEASE, RECOGNITION MOTIF, NERVOUS-SYSTEM, HUR, CANCER, DROSOPHILA, IDENTIFICATION

ID: 50081058